NVP-QAV680|CRTh2 receptor antagonist|DC Chemicals

NVP-QAV680|CRTh2 receptor antagonist|DC Chemicals

NVP-QAV680 is a potent and selective CRTh2 receptor antagonist with Ki of 36 nM by 3H-PGD2 filtration binding assay.

Product name: NVP-QAV680 |Cat No. DC8221|Other names: NVP-QAV680,NVPQAV680|Cas: 872365-16-7|Molecule Weight: 358.41|Molecule Formular: C18H18N2O4S| Purity: >98%

NVP-QAV680 is a potent and selective CRTh2 receptor antagonist with Ki of 36 nM by 3H-PGD2 filtration binding assay.
NVP-QAV680 is a highly selective compound  with low nM functional potency for inhibition of CRTh2 driven human eosinophil and Th2 lymphocyte activation in vitro. The molecule exhibited good oral bioavailability in the rat, combined with efficacy in rodent CRTh2-dependent mechanistic and allergic disease models and was suitable for clinical development.
in vitro: NVP-QAV680 was found to be inactive against eotaxin stimulated shape change mediated through the CCR-3 receptor. NVP-QAV680 elicited a potent inhibitory response to shape change elicited by both PGD2 and DK-PGD2 in whole blood. NVP-QAV680 exhibited nM potency for the blockade of DK-PGD2 induced IL-5 and IL-13 cytokine production from primary cultured human CD4+ Th2 lymphocytes.
in vivo: NVP-QAV680 dosed orally in an adapted variant of this model showed statistically significant inhibition of eosinophil infiltration after bronchoalveolar lavage (BAL) at a minimum dose of 1 mg/kg, with a trend to dose-dependency, thus confirming CRTh2 target engagement with a readout in a disease relevant tissue. In a follow up experiment, NVP-QAV680 was applied at lower doses of 0.3 and 0.1 mg/kg, with plasma sampling concomitant with BAL determination.

For research and scientific purpose only, not for human use.